Pyrimidine derivatives for the treatment of viral infections
This invention relates to pyrimidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections such as HCV or HBV.
1. A compound of formula (I)
or a pharmaceutically acceptable salt, tautomer(s), solvate or polymorph thereof, wherein
R 1 is hydrogen, C 1-4 alkyl, cyclopropyl, C 1-6 alkoxy, halogen, hydroxyl, or trifluoromethyl;
R 2 is C 1-8 alkyl optionally substituted by one or more substituents independently selected from the group consisting of halogen, hydroxyl, amino, C 1-6 alkyl, di-(C 1-6 )alkylamino, C 1-6 alkylamino, C 1-6 alkoxy, C 3-6 cycloalkyl, carboxylic acid, carboxylic ester, carboxylic amide, heterocycle, aryl, alkenyl, alkynyl, arylalkyl, heteroaryl, heteroarylalkyl, and nitrile, wherein said aryl, heterocycle, or heteroaryl is further optionally substituted by C 1-3 alkyl, alkoxy, carboxylic ester or carboxylic amide;
and
R 3 is C 4-8 alkyl, C 4-8 alkoxy, C 2-6 alkenyl or C 2-6 alkynyl, each of which is optionally substituted by one or more substituents independently selected from the group consisting of halogen, hydroxyl, amino, C 1-3 alkyl, C 1-3 alkoxy or C 3-6 cycloalkyl, and nitrile.
2. A compound as claimed in claim 1 wherein R 3 is butyl or pentyl.
3. A compound as claimed in claim 1 wherein R 3 is C 4-8 alkyl substituted with hydroxyl.
4. A compound as claimed in claim 3 wherein R 3 is selected from the group consisting of:
5. A compound as claimed in claim 1 wherein R 1 is hydrogen or —CH 3 .
6. A compound as claimed in claim 1 wherein R 2 is arylalkyl or heteroarylalkyl, each of which is independently, optionally substituted by one or more substituents selected from the group consisting of C 1-3 alkyl, hydroxyl, alkoxy, nitrile, heterocycle and ester.
7. A compound of formula (I) according to claim 1 wherein R 2 is selected from the group consisting of:
each of which is optionally substituted with C 1-6 alkyl, hydroxyl, C 1-6 alkoxy, nitrile, heterocycle or ester.
8. A compound as claimed in claim 1 selected from the group consisting of:
9. A pharmaceutical composition comprising a compound as claimed in claim 1 or a pharmaceutically acceptable salt, tautomer, solvate or polymorph thereof, and one or more pharmaceutically acceptable excipients, diluents or carriers.
10. A compound of claim 1 having the formula:
or a pharmaceutically acceptable salt, tautomer, solvate or polymorph thereof.
11. A compound of claim 1 having the formula:
or a pharmaceutically acceptable salt, tautomer, solvate or polymorph thereof.
12. A compound of claim 1 having the formula:
or a pharmaceutically acceptable salt, tautomer, solvate or polymorph thereof.
13. A pharmaceutical composition comprising the compound of claim 10 or a pharmaceutically acceptable salt, tautomer, solvate or polymorph thereof.
14. A pharmaceutical composition comprising the compound of claim 11 or a pharmaceutically acceptable salt, tautomer, solvate or polymorph thereof.
15. A pharmaceutical composition comprising the compound of claim 12 or a pharmaceutically acceptable salt, tautomer, solvate or polymorph thereof.